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Ophthalmic drug emulsion composition as well as preparation method and application thereof

A composition and emulsion technology, which is applied in drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of temperature sensitivity, poor reducibility, pain, etc., and achieve the effect of less stimulation, stable product performance, and improved stability

Pending Publication Date: 2022-06-07
山西利普达医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the above eye drops all increase the bioavailability by adding a thickener to physically thicken the mechanism, but when the viscosity increases to a certain value, the efficacy will not increase, and these bases have more Incompatibility, some are poorly reductive, some are Newtonian fluids, painful when blinking, sensitive to pH and / or temperature and unstable Lots of flaws

Method used

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  • Ophthalmic drug emulsion composition as well as preparation method and application thereof
  • Ophthalmic drug emulsion composition as well as preparation method and application thereof
  • Ophthalmic drug emulsion composition as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The compositions were prepared according to the components shown in Table 1, and three compositions of group 1, group 2 and group 3 were obtained respectively.

[0046] Table 1

[0047]

[0048] Preparation:

[0049] 1) Dissolve γ-cyclodextrin in water, add atropine sulfate, place it in an ultrasonic vibration cleaning machine, and ultrasonically mix for 30 minutes;

[0050] 2) Dissolve CKC, osmotic pressure regulator glycerol and tromethamine in the water phase;

[0051]3) Dissolve Polysorbate 80, Octoxynol 9, Tyloxapol or Poloxamer 188 in the oil phase;

[0052] 4) Heat the water phase and the oil phase to an appropriate temperature of 70-85°C, slowly pour the oil phase into the water phase under rapid mechanical stirring, continue stirring for 10 minutes, add water for injection to the full amount, and mix by high shear homogenization at least After 30 minutes, the oil droplets were reduced as much as possible, and the pH value was adjusted to 6.0 with dilute h...

Embodiment 2

[0054] The compositions were prepared according to the components shown in Table 2, and three compositions of group 4, group 5 and group 6 were obtained respectively.

[0055] Table 2

[0056]

[0057] Preparation:

[0058] 1) Weigh β-cyclodextrin and dissolve it in water, then add atropine, place it in an ultrasonic vibration cleaning machine, and ultrasonically mix for 30 minutes;

[0059] 2) Dissolve CKC, osmotic pressure regulator glycerol, boric acid and sodium borate in the water phase;

[0060] 3) Dissolve Polysorbate 80, Octoxynol 9, Tyloxapol or Poloxamer 188 in the oil phase;

[0061] 4) Heat the water phase and the oil phase to an appropriate temperature of 70-85°C, slowly pour the oil phase into the water phase under rapid mechanical stirring, continue stirring for 10 minutes, add water for injection to the full amount, and mix by high shear homogenization at least After 30 minutes, the oil droplets were reduced as much as possible, and the pH value was adjus...

Embodiment 3

[0063] The compositions were prepared according to the components shown in Table 3, and three compositions of group 7, group 8 and group 9 were obtained respectively.

[0064] table 3

[0065]

[0066] Preparation:

[0067] 1) Weigh α-cyclodextrin and dissolve it in water, then add atropine, put it in an ultrasonic vibration cleaning machine, and ultrasonically mix for 30 minutes;

[0068] 2) Dissolve CKC, osmotic pressure regulator glycerol, boric acid and sodium borate in the water phase;

[0069] 3) Dissolve Polysorbate 80, Octoxynol 9, Tyloxapol or Poloxamer 188 in the oil phase;

[0070] 4) Heat the water phase and the oil phase to an appropriate temperature of 70-85°C, slowly pour the oil phase into the water phase under rapid mechanical stirring, continue stirring for 10 minutes, add water for injection to the full amount, and mix by high shear homogenization at least For 30 minutes, the oil droplets were minimized, and the pH was adjusted to 4.0 with dilute hydro...

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Abstract

The invention discloses an ophthalmic medicine emulsion composition as well as a preparation method and application thereof. The ophthalmic drug emulsion composition comprises the following components in parts by weight: atropine sulfate and / or atropine accounting for 0.001%-1% of the total weight of the composition, an inclusion compound stabilizer accounting for 0.001%-18% of the total weight of the composition, hexadecyl dimethyl benzyl ammonium chloride accounting for 0.001%-0.1% of the total weight of the composition, an emulsifier accounting for 0.1%-4.0% of the total weight of the composition, and the balance of water. The oil phase accounts for 0.5%-2% of the total weight of the composition, the pH regulator accounts for 0.001%-0.25% of the total weight of the composition, the osmotic pressure regulator accounts for 0.5%-3.5% of the total weight of the composition, the chelating agent accounts for 0.001%-0.1% of the total weight of the composition, and the balance is water. The problem of stability of the atropine eye drops is solved, the bioavailability of the medicine is improved, the irritation to eyes is small, and the product performance is stable.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, relates to ophthalmic drugs, and in particular relates to an ophthalmic drug emulsion composition which can significantly improve the stability of a low-concentration atropine solution and a preparation method and application thereof. Background technique [0002] Clinical studies have confirmed that long-term atropine instillation can control the growth of diopter and axial length at the same time. The commonly used concentrations of atropine are 1%, 0.5%, 0.1%, 0.025%, 0.05%, 0.01%, etc., and its control effect on myopia is concentration-dependent The higher the concentration, the better the control effect, but the phenomenon of withdrawal withdrawal is also more obvious. There has also been increased concern about possible long-term side effects of 1% atropine eye drops, including phototoxic effects on the retina and lens, blurred near vision, photophobia, allergic reaction...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/46A61K47/18A61K47/69A61P27/02A61P27/06A61P27/10A61P37/08
CPCA61K9/107A61K9/0048A61K31/46A61K47/6951A61K47/186A61P27/10A61P27/02A61P37/08A61P27/06Y02A50/30
Inventor 李勇王稳定薛水玉秦爱方乔玉峰
Owner 山西利普达医药科技有限公司
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